anxiolytic-like effects

Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) is a naturally occurring monoterpene alcohol widely used in the production of perfumes and flavors.

TRIM (1-(2-Trifluoromethylphenyl)imidazole) is an inhibitor of nNOS.

SNAP 398299 is a Glycopeptide Receptor Type 3 (Gal3) antagonist with anxiolytic and antidepressant-like effects and is used in the study of mood disorders.

Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with antidepressant and anxiolytic-like effects.

Carpipramine (free base) is an atypical antipsychotic compound utilized in France and Japan to treat schizophrenia and anxiety. In addition to its neuroinhibitory and anxiolytic effects, it also possesses hypnotic properties. Structurally, carpipramine resembles tricyclic compounds like imipramine and is related to butyrophenones such as haloperidol.

Tracazolate (ICI 136,753) is a non-benzodiazepine compound that falls under the category of pyrazolo[1,6-a]pyridines and has demonstrated anxiolytic-like effects in animal models.

Dexmecamylamine ((+)-Mecamylamine) acts as an antagonist of nicotinic acetylcholine receptors (nAChR), effectively inhibiting α3β4, α4β2, α7, and α1β1γδ receptors, with an IC50 in the micromolar range. It also exhibits anxiolytic and antidepressant-like effects.

5-HT6R antagonist 3 (compound 15) is an effective and selective 5-HT6R antagonist capable of crossing the blood-brain barrier. It exhibits Ki values of 14 nM for 5-HT6, 3533 nM for 5-HT1A, 35 nM for 5-HT2A, and 1449 nM for 5-HT7. This compound demonstrates anxiolytic-like effects and possesses neuroprotective and cognitive-enhancing properties, indicating potential for Alzheimer's disease research.

Basimglurant (RG7090; RO4917523) sulfate is a selective, orally bioavailable negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5) that can cross the blood-brain barrier. It exhibits a Ki of 1.4 nM for [³H]-ABP688 and 35.6 nM for [³H]-MPEP. Basimglurant sulfate inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, modulates nucleus accumbens dopamine levels, and exerts anxiolytic, antidepressant-like, analgesic, and wakefulness-promoting effects, while altering δ-wave power during non-rapid eye movement sleep. It is applicable in research related to depression, fragile X syndrome, and anxiety disorders.

KRM-II-81 is a γ‑Aminobutyric Acid Type A (GABAA) Receptor Ligand. KRM-II-81 exhibits improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.

TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 |Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136255 PMID:26317356

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

Posovolone (Co 134444), an orally active neuroactive steroid with sedative-hypnotic properties, exhibits anticonvulsant and anxiolytic-like activities, alongside ataxic effects.

Neophytadiene is a diterpene compound extracted from Turbinaria ornate, with anti-inflammatory, antidepressant, anxiolytic-like, anticonvulsant, antioxidant, and cardioprotective effects. It inhibits LPS-induced inflammation in RAW 264.7 macrophages and Sprague-Dawley rats and can be used in neurological disease research.

NBI-31772 hydrate is a powerful inhibitor of the interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). It acts as a nonpeptide ligand, effectively releasing bioactive IGF-I from the IGF-I/IGFBP-3 complex (Ki values for all six human subtypes range from 1-24 nM). This compound demonstrates significant anxiolytic and antidepressant-like effects [1] [2] [3].

1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. 2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors. 3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.

MTEP, a potent, non-competitive, and highly selective antagonist of mGluR5, exhibits an IC50 value of 5 nM and a K_i value of 16 nM. Demonstrating antidepressant and anxiolytic-like effects, MTEP is utilized in Parkinson's disease research.

(S)-Osanetant, the S-enantiomer of Osanetant (SR142801), is a selective NK3 receptor antagonist known for its anxiolytic- and antidepressant-like effects. It is currently under investigation for potential use in treating schizophrenia [1].

Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective non-competitive inhibitor of TrkB, effectively impeding BDNF-triggered TrkB activity without altering BDNF binding affinity, with an IC50 of 0.30 nM. It crosses the blood-brain barrier, demonstrating analgesic and anxiolytic-like behavioral effects [1] [2] [3].

Phoenixin-20 (TFA) (PNX-20 (TFA)) is a bioactive peptide that stimulates hypothalamo-pituitary-gonadal hormones, regulates mammalian reproductive processes, enhances neuronal mitochondrial biogenesis via the CREB-PGC-1α pathway, and exhibits anxiolytic properties [1] [2] [3].

CP 122721 hydrochloride is a potent and selective non-peptide (nonpeptide) neurokinin NK1 antagonist, demonstrating a pIC50 of 9.8 against the human NK1 receptor in IM-9 cells. It exhibits anxiolytic and antidepressant-like effects, as evidenced in studies [1] [2].

Spinosin (Standard) is a reference standard for research and analysis in studies involving Spinosin. 1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. 2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors. 3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.

Mesembranol is an alkaloid identified in S. tortuosum with neuroinhibitory and anxiolytic-like effects. At concentrations of 17.16 and 34.32 nM, it reduces population spike amplitudes during theta burst stimulation in rat hippocampal slices. Additionally, Mesembranol (50 µM) enhances movement in the central arena in the light/dark preference test in zebrafish larvae, suggesting anxiolytic-like properties.